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English Abstract

Ophiopogonis Radix (Maidong in Chinese), the tuberous root of Ophiopogon japonicus, is widely used in traditional Chinese medicine (TCM). According to the TCM principle, Ophiopogonis Radix nourishes the yin, promotes body fluid production, moistens the lung, eases the mind and clears away heart fire. The main components of O.japonicus include steroidal saponins, homoisoflavonoids and polysaccharides, which exhibited various pharmacologic activities, such as cardiovascular protection, anti-inflammation, anticancer, anti-oxidation, immunomodulation, cough relief, antimicrobial, and anti-diabetes. In present study, quantitative analysis of 22 batches of O. japonicus from different regions and 4 batches of Liriope spicata var. prolifera was performed based on the chemical studies of O. japonicus, so as to better evaluate its quality. First, advance in the research of the botanical characteristics, chemical constituents, quality control, traditional uses, pharmacological activities about O.japonicus were reviewed in the dissertation. Column choromatography and Prep-HPLC were carried out for the isolation and purification of the constituents of O. japonicus. Eight compounds were isolated, and their structures were elucidated by means of MS, 1H-NMR and HPLC. They were identified as: ophiopogonanone C, β-sitosterol, methylophiopogonanone A, methylophiopogonanone B, palmitic acid, 1,3-bis(4-hydroxyphenyl)-1-propanone, ophiopogonin D and stigma-3-O-β-D-glucoside. Pressurized Liquid Extraction procedure (PLE) for O. japonicus was optimized. The parameters including the type of solvent, extraction temperature, static extraction time and times were studied by using univariate approach. Then an HPLC-DAD-ELSD method was developed for simultaneous determination of four saponins (ophiopogonin C, ophiopogonin D, liriopesides B, and ophiopogonin D'), four homoisoflavonoids (methylophiopogonone A, methylophiopogonone B, methylophiopogonanone A, and methylophiopogonanone B) and one sapogenin (ruscogenin) in O. japonicus. 14 v batches of O. japonicus from Sichuan (CMD), 8 batches of O. japonicus from Zhejiang (ZMD) and 4 batches of Liriope spicata var. prolifera (SMD) were analyzed and the results showed that the contents of the investigated compounds were greatly variant in O. japonicus from different regions and its substitute, Liriope spicata var. prolifera. Hierarchical clustering analysis based on contents of 9 investigated compounds showed that 26 samples were divided into three clusters: CMD, ZMD and SMD. Ophiopogonin D, methylophiopogonanone A, methylophiopogonanone B and liriopesides B were suggested as markers for differentiation of CMD, ZMD and SMD.

Chinese Abstract

麥冬為百合科植物麥冬 Ophiopogon japonicus(Thunb.)Ker-Gawl. 的乾燥塊 根,為常用的滋陰中藥,始載於《神農本草經》,具有養陰生津,潤肺清心的功 效,可用於治療熱病傷津,心煩口渴等病症。現代研究發現,麥冬的主要活性成 分為甾體皂苷、高異黃酮、多糖,具有保護心血管、抗炎、抗腫瘤、抗氧化、免 疫調節、鎮咳、抗微生物、抗糖尿病等多種生理藥理活性。為了對麥冬進行系統 的質量分析,建立有效的質量控制方法,本課題在對麥冬塊根的化學成分系統研 究的基礎上,對採集自不同產地的 22 批麥冬樣品,以及 4 批湖北麥冬樣品的主 要成分進行了含量測定。 首先對麥冬的植物特徵、化學成分、質量控制、傳統應用、藥理活性進行了 系統的綜述。 通過矽膠柱色譜、高效製備液相等分離手段對麥冬進行分離純化、從中分離 得到 8 個化合物,借助 MS、1H-NMR 等技術進行了結構鑒定,分別為:麥冬黃 烷酮 C,β-穀甾醇,甲基麥冬黃烷酮 A,甲基麥冬黃烷酮 B,棕櫚酸,1,3-bis(4- hydroxyphenyl)-1-propanone,麥冬皂苷 D 和豆甾醇-β-D-葡萄糖苷。 對麥冬的加壓溶劑提取條件進行了優化。對提取溶劑的種類,提取溫度,提 取時間和提取次數等進行了單因素考察,確定了麥冬藥材的加壓溶劑提取條件。 採用 HPLC-DAD-ELSD 法測定了麥冬中 4 個甾體皂苷(麥冬皂苷 C,麥冬 皂苷 D,山麥冬皂苷 B,麥冬皂苷 D'),4 個高異黃酮(甲基麥冬黃酮 A,甲基 麥冬黃酮 B,甲基麥冬黃烷酮 A,甲基麥冬黃烷酮 B)和 1 個皂苷元(魯斯可皂 苷元)的含量,並進行了方法學考察,對 26 批不同產地的麥冬樣品及其代用品 湖北麥冬進行了含量測定,並對結果進行了聚類分析,結果表明:不同產地麥冬 和湖北麥冬樣品的化學成分及含量具有較大差異,根據所測定 9 個成分的含量, 這 26 批樣品可分為川麥冬,浙麥冬和湖北麥冬三大類,其中麥冬皂苷 D、甲基 麥冬黃烷酮 A 和 B 以及山麥冬皂苷 B 分別為川麥冬、浙麥冬和湖北麥冬的特徵 性成分,可作為區分幾種麥冬類藥材的指標性成分。

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Institute of Chinese Medical Sciences




Plant bioactive compounds


Botanical chemistry


Materia medica -- China

藥物學 -- 中國



Lin, Li Gen

Chen, Xiao Jia

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